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Methods of treating lymphoma using thienotriazolodiazepine compounds

机译:噻吩并氮杂二氮杂卓类化合物治疗淋巴瘤的方法

摘要

A method of treating lymphoma in a mammal comprises the step of: administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5—(CH2)m—R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR7—CO—(CH2)q—R8 wherein R is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is —(CH2)a—CO—NH—R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or —(CH2)b—COOR10 wherein b is an integer of 1-4, and R10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof. The lymphoma to be treated is diffuse large B-cell lymphom (DLBCL) specifically selected from activated B-cell DLBCL (ABC-DLBCL) and germinal B-cell DLBCL (GBC-DLBCL).; embedded image
机译:一种治疗哺乳动物淋巴瘤的方法,其包括以下步骤:向患者施用药学上可接受量的化合物,所述化合物为式(1)的噻吩并三氮杂二氮杂pine化合物,其中R 1 是具有碳数的烷基在1-4中,R 2 是氢原子;卤素原子; R 3或S 8为碳原子数为1〜4的烷基,可任选被卤素原子或羟基取代。任选地被卤素原子取代的苯基,碳数为1-4的烷基,碳数为1-4的烷氧基或氰基; -NR 5 —(CH 2 m —R 6 其中R 5 是氢原子或碳数为1-4的烷基,m为0-4的整数,R 6是任选被卤素原子取代的苯基或吡啶基;或-NR 7 -CO-(CH 2 q -R 8 其中R是氢原子或碳数为1-4的烷基,n为0-2的整数,R 8 是苯基或吡啶基,可选地被卤素原子取代,R 4 是—(CH 2 a -CO-NH-R 9 ,其中a是1-4的整数,R 9 是碳数为1-4的烷基;碳数为1-4的羟烷基;碳数为1-4的烷氧基;或可任选地被碳数为1-4的烷基,碳数为1-4的烷氧基,氨基或羟基或-(CH 2 b <取代的苯基或吡啶基/ Sub> -COOR 10 其中b是1-4的整数,R 10 是碳数为1-4的烷基,或其药学上可接受的盐或其水合物或溶剂化物。要治疗的淋巴瘤是弥漫性大B细胞淋巴瘤(DLBCL),特别是选自活化B细胞DLBCL(ABC-DLBCL)和生发B细胞DLBCL(GBC-DLBCL)。 “嵌入式图像”

著录项

  • 公开/公告号US9968620B2

    专利类型

  • 公开/公告日2018-05-15

    原文格式PDF

  • 申请/专利权人 ONCOETHIX GMBH;

    申请/专利号US201515504722

  • 发明设计人 FRANCESCO BERTONI;

    申请日2015-08-19

  • 分类号A61K31/551;C07D487/12;C07D495/14;A61K45/06;A61K31/203;A61K31/4184;A61K31/436;A61K31/454;A61K31/519;A61K31/706;A61K38/07;

  • 国家 US

  • 入库时间 2022-08-21 13:00:13

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